Antineoplastic activity of two carbohydrate derivatives of chlorambucil in twohuman tumoral cell lines, MCF-7 of breast and KB-07 of naso pharyngeal

Resumen

Synthesis of two chlorambucil derivatives with junction to carbohydrate and liposolubleradicals was realized. The first compound is cyclohexyl 2-acetamido-3-o-(4-(4.[bis(2-chloro-ethyl)amino]phenyl)butanoyl)-2-deoxy-b- D-glucopyranosides, and the second com-pound is octyl 2-amino-2-N-(4-(4-[bis(2-chloroethyl)amino]phenyl) butanoyl)-2-deoxy-b-D-glucopyranoside. Treatment of cellular line MCF-7 with both compounds was realizedwith a trial of sulforrodamine B, and the survival, growth and citotoxicity rates whereanalysed. The effect of treatment in cellular line KB-07 with the above-mentionedcompounds, was quantified with a cytotoxicity study with Tryptan blue and the degree ofinhibition of cellular proliferation with the test of MTT. In the line MCF-7 of breast cancerthe first compound yielded a 73% survival rate and a 6.5% growth rate; it also showed tobe a inhibitor of cellular proliferation. On the contrary, the second compound had a 93.9%cytotoxicity rate and 4% survival rate and still was not an inhibitor of cellularproliferation, although it had strong cytotoxic action. The cellular line KB-07 ofnasopharyngeal carcinoma showed in regard to the first compound, with doses of 5 and20 lmol, a toxicity rate of 39.6% and 48.2%, meanwhile the second compound showed acytotoxicity rate of 24.8% and 36.4% respectively. The study of the inhibition of cellularproliferation was realized for the first compound in this line, obtaining for compound dosesof 10 and 20 lL, a inhibition rate of 23.8% and 37.8%, respectively. These in vitro resultsabout structural changes in the chlorambucil molecule, supports the need for newexperimental studies in animals (in vivo), as well as may be in the future is a phase Iclinical trial.